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BIFUNCTIONAL COMPOUND AND PHARMACEUTICAL COMPOSITION CAPABLE OF INDUCING DEGRADATION OF CORE SUBUNITS OF PRC2 PROTEIN COMPLEX, AND USE
BIFUNCTIONAL COMPOUND AND PHARMACEUTICAL COMPOSITION CAPABLE OF INDUCING DEGRADATION OF CORE SUBUNITS OF PRC2 PROTEIN COMPLEX, AND USE
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机译:能够诱导PRC2蛋白质复合物的核心亚基的降解的双官能化合物和药物组合物,并使用
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摘要
Disclosed are a bifunctional compound and a pharmaceutical composition capable of inducing the degradation of the core subunits of the PRC2 protein complex, and the use. The bifunctional compound comprises a compound as shown in any one of formulas I-III, a pharmaceutically acceptable salt or a prodrug thereof, a solvate thereof, a hydrate thereof, a polymorph thereof, a tautomer, a stereoisomer, or an isotope substituted compound thereof. In the formulas I-III, n is an integer of 1-10, X is O, N or S and Y is O, H2 or S. The bifunctional compound can induce the degradation of the core subunits of the PRC2 protein complex, thereby achieving the treatment of cancers mediated by PRC2 complex and subunits thereof, EZH2, EED, SUZ12, RbAp46 and RbAp48, and blocking the carcinogenic activity of the subunits of the PRC2 complex.
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